Synthesis, α-Glucosidase, α-Amylase, and Aldol Reductase Inhibitory Activity with Molecular Docking Study of Novel Imidazo[1,2-a]pyridine Derivatives

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dc.contributor.authorKaya, Betul
dc.contributor.authorCevik, Ulviye Acar
dc.contributor.authorCiftci, Bilge
dc.contributor.authorDuran, Hatice Esra
dc.contributor.authorTurkes, Cuneyt
dc.contributor.authorIsik, Mesut
dc.contributor.authorBostanci, Hayrani Eren
dc.date.accessioned2025-05-04T16:46:58Z
dc.date.available2025-05-04T16:46:58Z
dc.date.issued2024
dc.departmentSivas Cumhuriyet Üniversitesi
dc.description.abstractInhibition ofaldose reductase (AR), alpha-glycosidase (alpha-GLY), and alpha-amylase (alpha-AMY) are some of the essential targets in diabetes mellitus (DM). Here, a series of imidazo[1,2-a]pyridine-based 1,3,4-thiadiazole derivatives (8a-k) were successfully synthesized and characterized using 1H NMR, 13C NMR, and HRMS spectroscopic techniques. The inhibition effects of the synthesized derivatives against AR, alpha-GLY, and alpha-AMY were evaluated using both in vitro and in silico methods. In vitro studies revealed that the derivatives (8a-k) showed significant inhibition activity. The results showed that the novel derivatives (8a-k) demonstrated potential inhibitory activity, with K I values covering the following ranges: 23.47 +/- 2.40 to 139.60 +/- 13.33 nM for AR and 6.09 +/- 0.37 to 119.80 +/- 12.31 mu M for alpha-GLY, with IC50 values 81.14 to 153.51 mu M for alpha-AMY. Furthermore, many of these compounds exhibited high inhibition activity, while some of them showed higher potency than the reference compounds. Molecular docking of the target compounds was carried out in the active sites of AR (PDB ID: 4JIR) and alpha-GLY (PDB ID: 5NN8).
dc.description.sponsorshipThe authors present their thanks to Anadolu University for NMR spectra.
dc.identifier.doi10.1021/acsomega.4c05619
dc.identifier.endpage42914
dc.identifier.issn2470-1343
dc.identifier.issue42
dc.identifier.pmid39464438
dc.identifier.scopus2-s2.0-85206802391
dc.identifier.scopusqualityQ1
dc.identifier.startpage42905
dc.identifier.urihttps://doi.org/10.1021/acsomega.4c05619
dc.identifier.urihttps://hdl.handle.net/20.500.12418/35433
dc.identifier.volume9
dc.identifier.wosWOS:001332296900001
dc.identifier.wosqualityQ2
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakPubMed
dc.language.isoen
dc.publisherAmer Chemical Soc
dc.relation.ispartofAcs Omega
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.snmzKA_WOS_20250504
dc.subjectIdentification
dc.subjectDiscovery
dc.subjectHybrids
dc.subjectDesign
dc.titleSynthesis, α-Glucosidase, α-Amylase, and Aldol Reductase Inhibitory Activity with Molecular Docking Study of Novel Imidazo[1,2-a]pyridine Derivatives
dc.typeArticle

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